ARN-21934 is a potent, highly selective, and blood-brain barrier (BBB) penetrant inhibitor specifically targeting human topoisomerase IIα over β. It inhibits DNA relaxation with an IC50 of 2 μM, significantly more potent than the anticancer agent Etoposide (IC50=120 μM). The compound demonstrates a favorable in vivo pharmacokinetic profile and shows antiproliferative activity against various human cancer cell lines, making it a promising lead compound for anticancer research.
- Potent and highly selective topoisomerase IIα inhibitor
- Blood-brain barrier penetrant
- Inhibits DNA relaxation with IC50 of 2 μM
- Exhibits antiproliferative activity against human cancer cell lines
- Favorable in vivo pharmacokinetic profile
- Appears as a solid, light yellow to green yellow
- Soluble in DMSO (8.33 mg/mL at 80°C with ultrasonic)